Perspective

Fluorine in medicinal chemistry: a century of progress and a 60-year retrospective of selected highlights

† Author for correspondence

Department of Biological, Chemical, and Physical Sciences, Illinois Institute of Technology, Chicago, IL 60616, USA.

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Email the corresponding author at filler@iit.edu

Rituparna Saha

Department of Biological, Chemical, and Physical Sciences, Illinois Institute of Technology, Chicago, IL 60616, USA.

Search for more papers by this author

Email the corresponding author at filler@iit.edu

Published Online:19 Aug 2009https://doi.org/10.4155/fmc.09.65

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Abstract

This perspective explores the origins of both fluorine and medicinal chemistry a century ago and traces the early history of the intersection of these areas and the subsequent roles that fluorine has played in advancing medicinal innovations and diagnoses during the past 60 years. The overview highlights remarkable breakthroughs in many diverse areas of medicinal chemistry, including inter alia, anesthetics, steroidal and nonsteroidal anti-inflammatory drugs, anticancer and antiviral agents, CNS medications, antibacterials and cholesterol biosynthesis inhibitors. The increasing use of fluorine-18-labeled radiotracers in PET for diagnostic imaging of the brain, heart and in oncology is briefly presented. The signature roles of fluorine in medicinal chemistry are now firmly established. The presence of fluorine in pharmaceuticals has had a major impact on a plethora of important medical applications, such as those cited above. Fluorine will very likely continue to contribute significantly by playing multifaceted roles in enhancing future medical advances.

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Published online 19 August 2009

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Acknowledgements

The authors wish to express their thanks and appreciation to our spouses for their patience and understanding during the preparation of this article. Special thanks to Michael Filler–Knize for his valuable assistance in the preparation of the references.

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

No writing assistance was utilized in the production of this manuscript.

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